PEGYLATED GEMCITABINE AND METHOTREXATE: IN VITRO CYTOTOXICITY ANALYSIS AND IN VIVO DRUG RELEASE PROFILING TO ASSESS THEIR ENHANCED BLOOD CIRCULATION
Mahmood Ahmed · Acta Poloniae Pharmaceutica - Drug Research · 2019
In the present study, four new pegylated drugs were synthesized to investigate the anticancer activity.All the compounds were characterized on the basis of FTIR and 1 HNMR.The new compounds were evaluated against HCT116 cell line by CellTiter-GloÆ 3D cell viability assay.The sustained release pattern of newly synthesized compounds was also evaluated, slow-released lasts for 240 h which was confirmed by in vivo and in vitro drug release profile.The sustained and controlled release behavior of pegylated drugs over the extended period showed a linear profile and this release pattern was not limited to diffusion process instead supporting chemically controlled release pattern which was dependent only on how fast the compound hydrolyzed.The newly designed pegylated drugs showed almost the same killing effect against the cancer cells as free drugs.The compounds with lower cLogP value showed more antiproliferative (lower IC 50 ) effect due to their higher cell permeability.